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. Author manuscript; available in PMC: 2022 Aug 19.
Published in final edited form as: Pharmacol Rev. 2001 Dec;53(4):527–552.

TABLE 4.

Mutational analysis of the human A2B AR with respect to ligand binding

Mutationa Helix/Positionb Effect on Ligand Binding and Signal Transduction Reference
V11I 1.36 No changes in (radio)ligand binding Beukers et al., 2000
A12T 1.37 No changes in (radio)ligand binding Beukers et al., 2000
L58V 2.55 No changes in (radio)ligand binding Beukers et al., 2000
F59L 2.56 No specific radioligand binding and no cAMP production Beukers et al., 2000
N273Y 7.36 Up to 60-fold increase in affinity of 2-substituted adenosines Beukers et al., 2000
a

Amino acids are represented in single-letter code with position number shown. The first amino acid is that of the wild-type receptor, and the second is the one used for substitution, based on the corresponding amino acid in the human A2A receptor.

b

Position on helix, using notation of van Rhee and Jacobson (1996).